Molfile
Inchi
Smiles
Synonyms:
-
entecavir monohydrate
-
anhydrous entecavir
-
BMS-200475-01
-
entecavir
-
baraclude
-
entecavir hydrate
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Entecavir, a guanosine nucleoside analogue with activity against HBV reverse transcriptase, is efficiently phosphorylated to the active triphosphate form, which has an intracellular half-life of 15 hours. By competing with the natural substrate deoxyguanosine triphosphate, entecavir triphosphate functionally inhibits all three activities of the HBV reverse transcriptase: (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Entecavir triphosphate is a weak inhibitor of cellular DNA polymerases alpha, beta, and delta and mitochondrial DNA polymerase gamma with Ki values ranging from 18 to > 160 microM.
- Molecular weight: 277.28
- Formula: C12H15N5O3
- CLOGP: -1.78
- LIPINSKI: 0
- HAC: 8
- HDO: 4
- TPSA: 125.76
- ALOGS: -1.63
- ROTB: 2
- Status: OFP
Legend: OFP - off patent OFM - off market ONP - on patent
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